1383628-29-2

Upstream product

• 108-90-7 chlorobenzene 
• 25026-34-0 4-chlorophenacetyl chloride 
• 1383628-25-8 C₁₈H₁₃Cl₂NO₂S 
• 1383628-19-0 C₁₈H₁₃Cl₂NO₂ 
• 51490-05-2 1,2-bis(4-chlorophenyl)ethanone 
• 1878-66-6 4-chlorophenylacetic Acid 

Downstream Products

• 1437869-85-6 C₂₅H₁₇Cl₂NOS 
• 1437869-86-7 C₂₃H₁₅Cl₂NOS₂ 
• 1437869-87-8 C₂₃H₁₅Cl₂NO₂S 
• 1437869-88-9 C₃₂H₃₀Cl₂N₂O₂S 
• 1436572-80-3 C₂₁H₁₈Cl₂N₂OS 
• 1436572-88-1 C₂₂H₂₀Cl₂N₂OS 
• 1436573-02-2 C₂₃H₂₂Cl₂N₂O₂S 
• 1383627-63-1 C₂₂H₂₀Cl₂N₂OS 
• 1383627-32-4 C₂₃H₂₂Cl₂N₂OS 
• 1383627-39-1 C₂₂H₁₈Cl₂N₂O₂S 
• 1436574-16-1 C₂₄H₂₂Cl₂N₂O₂S 
• 1436574-22-9 C₂₉H₃₁Cl₂N₃O₃S 
• 1383627-43-7 C₂₂H₁₈Cl₂N₂O₂S 
• 1383627-41-5 C₂₂H₁₆Cl₂N₂O₃S 

Relevant academic research and scientific papers

Design, synthesis and biological evaluation of novel 3,4,5-trisubstituted aminothiophenes as inhibitors of p53-MDM2 interaction. Part 2

Five series of novel 3,4,5-trisubstituted aminothiophene derivatives and analogs were designed and synthesized based on our previous studies. All target compounds were evaluated for their p53-MDM2 binding inhibitory activities and anti-proliferation activities against A549 and PC3 tumor cell lines. Twelve compounds displayed comparable p53-MDM2 binding inhibitory activities to that of Nutlin-3. Among them, compound 7a exhibited marked binding affinity (IC 50 = 0.086 μM). In addition, most target compounds showed potent anti-proliferation activities with IC50 values at low micromolar level. A good selective profile for wild-type p53 expression cell line was also observed. Molecular docking analysis was performed as well to predict possible binding modes of target compounds with MDM2.

Design, synthesis and biological evaluation of novel 3,4,5-trisubstituted aminothiophenes as inhibitors of p53-MDM2 interaction. Part 1

A series of 3,4,5-trisubstituted aminothiophenes were designed, synthesized, and evaluated for their p53-MDM2 binding inhibitory potency and anti-proliferation activities against A549 and PC3 tumor cell lines. Fourteen compounds had appreciably improved MDM2 binding affinities than lead compound MCL0527 (3) and a few compounds showed comparable activities to that of Nutlin-3. Meanwhile, most of the 3,4,5-trisubstituted aminothiophenes displayed better or equivalent anti-proliferation activities against wild-type p53 cell line A549 compared to that of Nutlin-3. Over ten compounds exhibited desirable selective profiles of p53 status. Particularly, compounds 9, 16 and 18 displayed 22-, 6- and 22-fold selectivity of p53 status, respectively, much better than that of Nutlin-3 (fourfold).